Tetrabenazine transdermal delivery device
Inventors
Borsadia, Suresh • Patel, Kalpana • Tan, Hock S.
Assignees
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Publication Number
US-12144899-B2
Publication Date
2024-11-19
Expiration Date
Abstract
Provided herein are transdermal delivery devices comprising tetrabenazine, a deuterated tetrabenazine, or a combination thereof. Also provided herein are pharmaceutical compositions, such as adhesive compositions, comprising tetrabenazine, a deuterated tetrabenazine, or a combination thereof, for example, homogenously dispersed in an adhesive, such as a pressure sensitive adhesive. Further provided herein are methods of using the transdermal delivery devices or pharmaceutical compositions, for example, for treating a hyperkinetic movement disorder.
Core Innovation
The invention relates to an adhesive composition and a transdermal delivery device for dispersing tetrabenazine or deuterated tetrabenazine in a non-reactive acrylate pressure sensitive adhesive. The composition includes a crystallization inhibitor defined as a polyethylene glycol, polyvinyl acetate, and polyvinylcaprolactame based graft copolymer, and the non-reactive acrylate pressure sensitive adhesive is present in an amount of about 50% to about 97% by weight and does not have functional groups selected from epoxy, —OH, —COOH, and combinations thereof.
The transdermal delivery device includes a backing layer, the adhesive composition, and a release liner. The adhesive composition comprises tetrabenazine or deuterated tetrabenazine dispersed in a specified non-reactive acrylate pressure sensitive adhesive copolymer, and further includes the polyethylene glycol, polyvinyl acetate, and polyvinylcaprolactame-based graft copolymer crystallization inhibitor and propyl gallate.
The invention is directed to inhibiting VMAT2 by applying the adhesive composition of the device to the skin of a subject, thereby addressing hyperkinetic movement disorders. Documented use cases include chronic hyperkinetic movement disorders such as chorea associated with Huntington’s disease, tardive dyskinesia, Wilson’s disease, Tourette syndrome, and restless leg syndrome.
Claims Coverage
The partial content includes two independent claims: one directed to an adhesive composition and one directed to a transdermal delivery device. Each independent claim contains multiple inventive features, including selection of the active ingredient, formulation into a non-reactive acrylate pressure sensitive adhesive, inclusion of a defined crystallization inhibitor, and, for the device claim, inclusion of propyl gallate and specified device layers.
Non-reactive acrylate pressure sensitive adhesive for tetrabenazine
An active ingredient selected from tetrabenazine, deuterated tetrabenazine, or a combination thereof dispersed in a non-reactive acrylate pressure sensitive adhesive, wherein the adhesive is present in an amount of about 50% to about 97% by weight and does not have functional groups selected from epoxy, —OH, —COOH, and combinations thereof.
Crystallization inhibitor with PEG/PVAc/PVCap graft copolymer
A crystallization inhibitor which is a polyethylene glycol, polyvinyl acetate, and polyvinylcaprolactame based graft copolymer.
Transdermal delivery device with backing layer and release liner
A transdermal delivery device comprising a backing layer, an adhesive composition, and a release liner, wherein the adhesive composition comprises tetrabenazine, deuterated tetrabenazine, or a combination thereof dispersed in a non-reactive acrylate pressure sensitive adhesive copolymer, a crystallization inhibitor being a polyethylene glycol, polyvinyl acetate, and polyvinylcaprolactame-based graft copolymer, and propyl gallate.
Defined weight ranges including propyl gallate for the device adhesive
The adhesive composition comprises by weight percentage about 2% to about 10% active ingredient, about 50% to about 90% non-reactive acrylate pressure sensitive adhesive, about 5% to about 40% crystallization inhibitor, and about 0.001% to about 0.5% propyl gallate.
Overall, the claim coverage centers on formulating tetrabenazine or deuterated tetrabenazine in a non-reactive acrylate pressure sensitive adhesive lacking epoxy, —OH, and —COOH functional groups, combined with a PEG/PVAc/PVCap graft copolymer crystallization inhibitor. The transdermal device claim further specifies a backing layer, release liner, propyl gallate, and defined weight-percentage ranges for the adhesive composition.
Stated Advantages
Avoid first-pass metabolism compared to oral dosing.
Reduce Cmax and inter-individual variability compared to oral dosing.
Potentially simplify CYP2D6-genotyping.
Improve shelf stability by preventing drug crystals after shelf storage.
No drug degradation detected by HPLC after shelf storage.
Documented Applications
Inhibiting VMAT2 in a subject by applying the adhesive composition to the skin of the subject.
Treatment of chronic hyperkinetic movement disorders, including chorea associated with Huntington’s disease, tardive dyskinesia, Wilson’s disease, Tourette syndrome, and restless leg syndrome.
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